Примери за използване на Trifluridine на Английски и техните преводи на Български
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Trifluridine stops the growth of cancer cells.
The active substances are trifluridine and tipiracil.
Trifluridine is a substrate of TPase, but is not metabolised by cytochrome P450(CYP).
Each tablet contains 15 mg trifluridine and 6.14 mg tipiracil.
NAME OF THE MEDICINAL PRODUCT Lonsurf 20 mg/8.19 mg film-coated tablets trifluridine/tipiracil.
Tipiracil increases the level of trifluridine in the blood by slowing its breakdown.
Trifluridine was mainly eliminated by metabolism via TPase to form an inactive metabolite, FTY.
Lonsurf contains two different active substances: trifluridine and tipiracil.
Toxicology assessment of trifluridine/tipiracil hydrochloride was performed in rats, dogs and monkeys.
Estimated(CrCl) was a significant covariate for CL/F in both final models of trifluridine and tipiracil hydrochloride.
In vitro studies indicated that trifluridine is a substrate for the nucleoside transporters CNT1, ENT1 and ENT2.
Such medicinal products,if used concomitantly with Lonsurf, may compete with the effector, trifluridine, for activation via thymidine kinases.
Based on findings in animals, trifluridine may cause foetal harm when administered to pregnant women.
STATEMENT OF ACTIVE SUBSTANCE(S) Each film-coated tablet contains 15 mg trifluridine and 6.14 mg of tipiracil(as hydrochloride).
In the body, trifluridine is converted into an active form that is incorporated into DNA, the genetic material of cells.
Each film-coated tablet contains 20 mg trifluridine and 8.19 mg tipiracil(as hydrochloride).
As a result, trifluridine interferes with DNA function and prevents the cells from dividing to make more cells.
Serum albumin was found to significantly affect trifluridine clearance, with a negative correlation.
Thus trifluridine and tipiracil hydrochloride are not expected to cause or be subject to a significant medicinal product interaction mediated by CYP.
Twelve-month OS rates were 21.2% in the trifluridine/tipiracil group and 13.0% in the placebo group.
Tipiracil stops the trifluridine from being broken down by the body, helping trifluridine to work longer.
No long term studies evaluating the carcinogenic potential of trifluridine/tipiracil hydrochloride in animals have been performed.
In nonclinical studies, trifluridine/tipiracil hydrochloride demonstrated antitumour activity against both 5-fluorouracil(5-FU) sensitive and resistant colorectal cancer cell lines.
As for the other exposure parameters of trifluridine and tipiracil hydrochloride, those appeared to be dose proportional.
The protein binding of trifluridine in human plasma was over 96% and trifluridine bound mainly to human serum albumin.
Results of animal studies did not indicate an effect of trifluridine and tipiracil hydrochloride on male and female fertility in rats.
In vitro studies indicated that trifluridine, tipiracil hydrochloride and 5-[trifluoromethyl] uracil(FTY) did not inhibit the activity of human cytochrome P450(CYP) isoforms.
When Lonsurf at a single dose of 35 mg/m2 was administered to 14 patients with solid tumoursafter a standardised high-fat, high-calorie meal, trifluridine area under the concentration-time curve(AUC) did not change, but trifluridine Cmax, tipiracil hydrochloride Cmax and AUC decreased by approximately 40% compared to those in a fasting state.
Based on the mechanism of action, trifluridine is suspected to cause congenital malformations when administered during pregnancy.
Studies in animals have shown excretion of trifluridine, tipiracil hydrochloride and/or their metabolites in milk(see section 5.3).